1. GPCR/G Protein Neuronal Signaling
  2. Dopamine Receptor
  3. ABT-724 trihydrochloride

ABT-724 trihydrochloride  (Synonyms: ABT-724三塩酸塩)

製品番号: HY-103409 純度: 99.05%
COA 取扱説明書 Technical Support

ABT-724 trihydrochloride is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 trihydrochloride is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM), and has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 trihydrochloride could be useful for the treatment of erectile dysfunction and has favorable side-effect profile.

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ABT-724 trihydrochloride

ABT-724 trihydrochloride 構造式

CAS 番号 : 587870-77-7

容量 価格(税別) 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 45 在庫あり
Solution
10 mM * 1 mL in DMSO USD 45 在庫あり
Solid
5 mg $41 在庫あり
10 mg $71 在庫あり
25 mg $154 在庫あり
50 mg $238 在庫あり
100 mg $356 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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製品説明

ABT-724 trihydrochloride is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 trihydrochloride is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM), and has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 trihydrochloride could be useful for the treatment of erectile dysfunction and has favorable side-effect profile[1].

IC50 & Target

D4 Receptor

 

体外実験

ABT-724 exhibits a selective biochemical profile, as indicates by a lack of binding affinity for >70 neurotransmitter/uptake/ion channels including D2, D3, or D5 receptors up to a 10 μM concentration. A weak affinity to 5-HT1A receptors (Ki = 2780 nM) is observed. ABT-724 does not inhibit the PDE activity of PDE1, PDE5, or PDE6 at 10 μM concentrations[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

ABT-724 (8.8 μg/kg; subcutaneous injection; daily; for 5 days; male adult Wistar rats) treatment dose-dependently facilitates penile erection when given s.c. to conscious rats[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male adult Wistar rats (~300 g)[1]
Dosage: 8.8 μg/kg
Administration: Subcutaneous injection; daily; for 5 days
Result: Dose-dependently facilitated penile erection.
分子量

402.75

分子式

C17H22Cl3N5

CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

[H]Cl.[H]Cl.[H]Cl.C1(NC(CN2CCN(C3=NC=CC=C3)CC2)=N4)=C4C=CC=C1

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶剤 & 溶解度
体外: 

H2O : ≥ 100 mg/mL (248.29 mM)

DMSO : 20 mg/mL (49.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4829 mL 12.4146 mL 24.8293 mL
5 mM 0.4966 mL 2.4829 mL 4.9659 mL
10 mM 0.2483 mL 1.2415 mL 2.4829 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始)

C1

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体積 (開始)

V1

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C2

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体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.21 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.21 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 100 mg/mL (248.29 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
純度とドキュメンテーション

純度: 99.05%

参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 2.4829 mL 12.4146 mL 24.8293 mL 62.0732 mL
5 mM 0.4966 mL 2.4829 mL 4.9659 mL 12.4146 mL
10 mM 0.2483 mL 1.2415 mL 2.4829 mL 6.2073 mL
15 mM 0.1655 mL 0.8276 mL 1.6553 mL 4.1382 mL
20 mM 0.1241 mL 0.6207 mL 1.2415 mL 3.1037 mL
25 mM 0.0993 mL 0.4966 mL 0.9932 mL 2.4829 mL
30 mM 0.0828 mL 0.4138 mL 0.8276 mL 2.0691 mL
40 mM 0.0621 mL 0.3104 mL 0.6207 mL 1.5518 mL
H2O 50 mM 0.0497 mL 0.2483 mL 0.4966 mL 1.2415 mL
60 mM 0.0414 mL 0.2069 mL 0.4138 mL 1.0346 mL
80 mM 0.0310 mL 0.1552 mL 0.3104 mL 0.7759 mL
100 mM 0.0248 mL 0.1241 mL 0.2483 mL 0.6207 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
× = ×
C1   V1   C2   V2
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製品名:
ABT-724 trihydrochloride
製品番号:
HY-103409
数量:
MCE 日本正規代理店: